A-443654
- Product Name
- A-443654
- CAS No.
- 552325-16-3
- Chemical Name
- A-443654
- Synonyms
- A-443654;A-443654 ,E1125;A-443654;A443654;A-443654, 10 mM in DMSO;inhibit,A443654,A-443654,Inhibitor,PKB,Akt,A 443654,Protein kinase B;(2S)-1-(1H-indol-3-yl)-3-[5-(3-methyl-2H-indazol-5-yl)pyridin-3-yl]oxypropan-2-amine;(S)-1-(1H-Indol-3-yl)-3-((5-(3-methyl-1H-indazol-5-yl)pyridin-3-yl)oxy)propan-2-amine;1H-Indole-3-ethanamine, α-[[[5-(3-methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]-, (αS)-;1H-Indole-3-ethanaMine, a-[[[5-(3-Methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]Methyl]-, (aS)-;(alphaS)-alpha-[[[5-(3-Methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]-(S)-1H-indole-3-ethanamine
- CBNumber
- CB92627239
- Molecular Formula
- C24H23N5O
- Formula Weight
- 397.47
- MOL File
- 552325-16-3.mol
A-443654 Property
- Boiling point:
- 722℃
- Density
- 1.307
- Flash point:
- 390℃
- storage temp.
- Store at -20°C
- solubility
- insoluble in H2O; ≥19.85 mg/mL in DMSO; ≥44.3 mg/mL in EtOH
- form
- solid
- pka
- 13.43±0.40(Predicted)
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- 16499
- Product name
- A-443654
- Purity
- ≥98%
- Packaging
- 500μg
- Price
- $68
- Updated
- 2024/03/01
- Product number
- 16499
- Product name
- A-443654
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $109
- Updated
- 2024/03/01
- Product number
- 16499
- Product name
- A-443654
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $401
- Updated
- 2024/03/01
- Product number
- INB0001420
- Product name
- A-443654
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $503.87
- Updated
- 2021/12/16
- Product number
- orb611401
- Product name
- A-443654
- Packaging
- 5mg
- Price
- $569.5
- Updated
- 2021/12/16
A-443654 Chemical Properties,Usage,Production
Uses
A-443654 is a pan-Akt inhibitor and has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM)[1].
Definition
ChEBI: (2S)-1-(1H-indol-3-yl)-3-[[5-(3-methyl-2H-indazol-5-yl)-3-pyridinyl]oxy]-2-propanamine is a member of indoles.
in vivo
A-443654 (7.5 mg/kg/d, s.c.) inhibits tumor growth in the 3T3-Akt1 flank tumor model. A-443654 (50 mg/kg, s.c.) induces apoptosis in 3T3-Akt1 flank tumors. A-443654 (30 mg/kg, s.c.) leads to increased levels of phosphorylated Akt1 in MiaPaCa-2 tumors[1].
target
Akt1
IC 50
Akt1: 160 pM (Ki); Akt2: 160 pM (Ki); Akt3: 160 pM (Ki); PKA: 6.3 nM (Ki); RSK2: 11 nM (Ki); PKCγ: 24 nM (Ki); CDK2: 24 nM (Ki); PKCδ: 33 nM (Ki); GSK3β: 41 nM (Ki); ERK2: 340 nM (Ki); cKIT: 1.2 μM (Ki); Chk1: 2.3 μM (Ki); CK2: 2.4 μM (Ki); SRC: 2.6 μM (Ki); KDR: 3.1 μM (Ki); MAPK-AP2: 3.3 μM (Ki); Flt1: 3.6 μM (Ki)
References
[1] Luo Y, et al. Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo. Mol Cancer Ther. 2005 Jun;4(6):977-86. DOI:10.1158/1535-7163.MCT-05-0005
[2] Zheng J, et al. Rapamycin sensitizes Akt inhibition in malignant human breast epithelial cells. Cancer Lett. 2010 Oct 1;296(1):74-87. DOI:10.1016/j.canlet.2010.03.018
[3] Gallia GL, et al. Inhibition of Akt inhibits growth of glioblastoma and glioblastoma stem-like cells. Mol Cancer Ther. 2009 Feb;8(2):386-93. DOI:10.1158/1535-7163.MCT-08-0680
[4] Zhao Y, et al. Estrogen receptor alpha and beta regulate actin polymerization and spatial memory through an SRC-1/mTORC2-dependent pathway in the hippocampus of female mice. J Steroid Biochem Mol Biol. 2017 Nov;174:96-113. DOI:10.1016/j.jsbmb.2017.08.003
A-443654 Preparation Products And Raw materials
Raw materials
Preparation Products
A-443654 Suppliers
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View Lastest Price from A-443654 manufacturers
- Product
- A-443654 552325-16-3
- Price
- US $2.00-5.00/KG
- Min. Order
- 0.1KG
- Purity
- 99%
- Supply Ability
- g-kg-tons
- Release date
- 2025-07-10
- Product
- A-443654 552325-16-3
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 98%
- Supply Ability
- 1lg; 2kg; 5kg; 10kg; 100kg
- Release date
- 2019-08-31